PT2576548E - Utilização de estimuladores de sgc, activadores de sgc, por si sós ou em combinação com inibidores de pde5 para o tratamento de esclerose sistémica (sgc) - Google Patents

Utilização de estimuladores de sgc, activadores de sgc, por si sós ou em combinação com inibidores de pde5 para o tratamento de esclerose sistémica (sgc) Download PDF

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Publication number
PT2576548E
PT2576548E PT117227868T PT11722786T PT2576548E PT 2576548 E PT2576548 E PT 2576548E PT 117227868 T PT117227868 T PT 117227868T PT 11722786 T PT11722786 T PT 11722786T PT 2576548 E PT2576548 E PT 2576548E
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Portugal
Prior art keywords
sgc
ssc
alone
combinations
treatment
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PT117227868T
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English (en)
Portuguese (pt)
Inventor
Stasch Dr Johannes-Peter
Claudia Hirth-Dietrich
Andreas Knorr
Peter Sandner
Georges Von Degenfeld
Markus Follmann
Michael Hahn
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Adverio Pharma Gmbh
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Priority claimed from DE102010021637A external-priority patent/DE102010021637A1/de
Application filed by Adverio Pharma Gmbh filed Critical Adverio Pharma Gmbh
Publication of PT2576548E publication Critical patent/PT2576548E/pt

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/38Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
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    • C07D261/10Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D487/04Ortho-condensed systems

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  • Life Sciences & Earth Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
PT117227868T 2010-05-26 2011-05-24 Utilização de estimuladores de sgc, activadores de sgc, por si sós ou em combinação com inibidores de pde5 para o tratamento de esclerose sistémica (sgc) PT2576548E (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102010021637A DE102010021637A1 (de) 2010-05-26 2010-05-26 Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
EP10170413 2010-07-22

Publications (1)

Publication Number Publication Date
PT2576548E true PT2576548E (pt) 2015-09-16

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PT117227868T PT2576548E (pt) 2010-05-26 2011-05-24 Utilização de estimuladores de sgc, activadores de sgc, por si sós ou em combinação com inibidores de pde5 para o tratamento de esclerose sistémica (sgc)

Country Status (31)

Country Link
US (1) US10189856B2 (hr)
EP (1) EP2576548B1 (hr)
JP (1) JP5883852B2 (hr)
KR (1) KR101881174B1 (hr)
CN (1) CN103038232B (hr)
AU (1) AU2011257336B2 (hr)
CA (2) CA2800709C (hr)
CL (1) CL2012003281A1 (hr)
CR (1) CR20120597A (hr)
CY (1) CY1116703T1 (hr)
DK (1) DK2576548T3 (hr)
EA (1) EA030735B9 (hr)
ES (1) ES2549979T3 (hr)
HK (1) HK1183868A1 (hr)
HR (1) HRP20150987T1 (hr)
HU (1) HUE025162T2 (hr)
IL (1) IL223128A (hr)
MA (1) MA34249B1 (hr)
ME (1) ME02207B (hr)
MX (1) MX2012013574A (hr)
MY (1) MY170094A (hr)
NZ (1) NZ603799A (hr)
PL (1) PL2576548T3 (hr)
PT (1) PT2576548E (hr)
RS (1) RS54261B1 (hr)
SG (1) SG185690A1 (hr)
SI (1) SI2576548T1 (hr)
TN (1) TN2012000550A1 (hr)
UA (1) UA116521C2 (hr)
WO (1) WO2011147810A1 (hr)
ZA (1) ZA201208824B (hr)

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DE102010021637A1 (de) * 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
RS54261B1 (en) 2010-05-26 2016-02-29 Adverio Pharma Gmbh USE OF SGC STIMULATORS, SGC ACTIVATORS, INDIVIDUALLY AND IN COMBINATION WITH PDE5 INHIBITORS FOR SYSTEMIC SCLEROSIS TREATMENT (SSC)
RU2582679C2 (ru) 2010-11-09 2016-04-27 Айронвуд Фармасьютикалз, Инк. СТИМУЛЯТОРЫ sGC
EP2594270A3 (en) * 2011-11-18 2013-07-31 BIP Patents The use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of systemic sclerosis (SSc)
CN102491974B (zh) 2011-12-12 2013-08-07 南京药石药物研发有限公司 1-(2-氟苄基)-1H-吡唑并[3,4-b]吡啶-3-甲脒盐酸盐的合成方法
US9139564B2 (en) 2011-12-27 2015-09-22 Ironwood Pharmaceuticals, Inc. 2-benzyl, 3-(pyrimidin-2-yl) substituted pyrazoles useful as sGC stimulators
WO2013131923A1 (de) * 2012-03-06 2013-09-12 Bayer Intellectual Property Gmbh Substituierte azabicyclen und ihre verwendung
NZ703989A (en) * 2012-09-07 2017-04-28 Boehringer Ingelheim Int Alkoxy pyrazoles as soluble guanylate cyclase activators
WO2014047325A1 (en) * 2012-09-19 2014-03-27 Ironwood Pharmaceuticals, Inc. Sgc stimulators
MX2015010725A (es) * 2013-02-21 2016-05-31 Adverio Pharma Gmbh Formas de metil {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo [3,4-b] piridino-3-il] pirimidino-5-il} metil carbamato.
US9452170B2 (en) 2013-03-15 2016-09-27 The California Institute For Biomedical Research Compounds and methods for inducing chondrogenesis
WO2015011086A1 (en) 2013-07-25 2015-01-29 Bayer Pharma Aktiengesellschaft Sgc stimulators or sgc activators and pde5 inhibitors in combination with additional treatment for the therapy of cystic fibrosis
WO2015056663A1 (ja) * 2013-10-15 2015-04-23 トーアエイヨー株式会社 4-アミノメチル安息香酸誘導体
WO2015106268A1 (en) 2014-01-13 2015-07-16 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
KR102347721B1 (ko) 2014-06-13 2022-01-05 엥방티바 섬유성 질환의 치료에 사용하기 위한 ppar 화합물
TW201625584A (zh) 2014-07-02 2016-07-16 諾華公司 茚滿及吲哚啉衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途
MX2017000926A (es) 2014-07-22 2017-05-04 Boehringer Ingelheim Int Acidos carboxilicos heterociclicos como activadores de guanilato ciclasa soluble.
AU2016258847A1 (en) 2015-05-06 2017-11-16 Bayer Pharma Aktiengesellschaft The use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of Digital Ulcers (DU) concomitant to Systemic Sclerosis (SSc)
DK3325013T4 (da) * 2015-07-23 2023-10-16 Bayer Pharma AG Stimulatorer og/eller aktivatorer af den opløselige guanylatcyklase (sgc) i kombination med en inhibitor af den neutrale endopeptidase (nep inhibitor) og en angiotensin aii-antagonist og deres anvendelse
JP7153331B2 (ja) * 2015-10-07 2022-10-14 アイビバ バイオファーマ インコーポレイテッド 皮膚線維性障害を治療するための組成物
EA201891416A1 (ru) 2015-12-14 2018-12-28 Айронвуд Фармасьютикалз, Инк. ПРИМЕНЕНИЕ СТИМУЛЯТОРОВ sGC ДЛЯ ЛЕЧЕНИЯ ДИСФУНКЦИИ ЖЕЛУДОЧНО-КИШЕЧНОГО СФИНКТЕРА
WO2017103888A1 (en) 2015-12-18 2017-06-22 Novartis Ag Indane derivatives and the use thereof as soluble guanylate cyclase activators
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